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Assay Detail

CHEMBL645926

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Binding
In vitro inhibition of Acyl coenzyme A:cholesterol acyltransferase in rat hepatic microsomes
ChEMBL ↗
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Microsomes
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sterol O-acyltransferase 1 (CHEMBL285) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: synthesis and structure-activity relationship studies of a new series of trisubstituted imidazoles.
Higley CA, Wilde RG, Maduskuie TP, Johnson AL, Pennev P, Billheimer JT, Robinson CS, Gillies PJ, Wexler RR.
J Med Chem (1994) 37 : 3511 -3522
PubMed 7932580 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 53 7.02 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL119295 — — 1 8.10
CHEMBL115514 — — 1 8.10
CHEMBL119484 — — 1 8.00
CHEMBL119678 — — 1 8.00
CHEMBL333013 — — 1 8.00
CHEMBL274185 LECIMIBIDE 2.0 1 8.00
CHEMBL326364 — — 1 7.80
CHEMBL331023 — — 1 7.80
CHEMBL119369 — — 1 7.70
CHEMBL119169 — — 1 7.70
CHEMBL119759 — — 1 7.70
CHEMBL119729 — — 1 7.64
CHEMBL334218 — — 1 7.60
CHEMBL116093 — — 1 7.52
CHEMBL119606 — — 1 7.52
CHEMBL119645 — — 1 7.52
CHEMBL119081 — — 1 7.52
CHEMBL115682 — — 1 7.52
CHEMBL115686 — — 1 7.52
CHEMBL119271 — — 1 7.47
CHEMBL119751 — — 1 7.40
CHEMBL332967 — — 1 7.40
CHEMBL117919 — — 1 7.40
CHEMBL332389 — — 1 7.30
CHEMBL326045 — — 1 7.30
CHEMBL333653 — — 1 7.30
CHEMBL323894 — — 1 7.24
CHEMBL118701 — — 1 7.22
CHEMBL120285 — — 1 7.16
CHEMBL333504 — — 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL119295 — IC50 = 8.0 nM 8.10
CHEMBL115514 — IC50 = 8.0 nM 8.10
CHEMBL119678 — IC50 = 10.0 nM 8.00
CHEMBL333013 — IC50 = 10.0 nM 8.00
CHEMBL274185 LECIMIBIDE IC50 = 10.0 nM 8.00
CHEMBL119484 — IC50 = 10.0 nM 8.00
CHEMBL326364 — IC50 = 16.0 nM 7.80
CHEMBL331023 — IC50 = 16.0 nM 7.80
CHEMBL119369 — IC50 = 20.0 nM 7.70
CHEMBL119169 — IC50 = 20.0 nM 7.70
CHEMBL119759 — IC50 = 20.0 nM 7.70
CHEMBL119729 — IC50 = 23.0 nM 7.64
CHEMBL334218 — IC50 = 25.0 nM 7.60
CHEMBL115686 — IC50 = 30.0 nM 7.52
CHEMBL119606 — IC50 = 30.0 nM 7.52
CHEMBL119645 — IC50 = 30.0 nM 7.52
CHEMBL119081 — IC50 = 30.0 nM 7.52
CHEMBL116093 — IC50 = 30.0 nM 7.52
CHEMBL115682 — IC50 = 30.0 nM 7.52
CHEMBL119271 — IC50 = 34.0 nM 7.47
CHEMBL119751 — IC50 = 40.0 nM 7.40
CHEMBL332967 — IC50 = 40.0 nM 7.40
CHEMBL117919 — IC50 = 40.0 nM 7.40
CHEMBL333653 — IC50 = 50.0 nM 7.30
CHEMBL332389 — IC50 = 50.0 nM 7.30
CHEMBL326045 — IC50 = 50.0 nM 7.30
CHEMBL323894 — IC50 = 58.0 nM 7.24
CHEMBL118701 — IC50 = 60.0 nM 7.22
CHEMBL120285 — IC50 = 70.0 nM 7.16
CHEMBL333504 — IC50 = 70.0 nM 7.16
CHEMBL119586 — IC50 = 70.0 nM 7.16
CHEMBL420356 — IC50 = 80.0 nM 7.10
CHEMBL331131 — IC50 = 80.0 nM 7.10
CHEMBL119272 — IC50 = 100.0 nM 7.00
CHEMBL332705 — IC50 = 150.0 nM 6.82
CHEMBL332522 — IC50 = 160.0 nM 6.80
CHEMBL325036 — IC50 = 170.0 nM 6.77
CHEMBL119644 — IC50 = 200.0 nM 6.70
CHEMBL325663 — IC50 = 200.0 nM 6.70
CHEMBL332487 — IC50 = 230.0 nM 6.64
CHEMBL115698 — IC50 = 280.0 nM 6.55
CHEMBL118231 — IC50 = 400.0 nM 6.40
CHEMBL48034 — IC50 = 490.0 nM 6.31
CHEMBL119362 — IC50 = 510.0 nM 6.29
CHEMBL332966 — IC50 = 910.0 nM 6.04
CHEMBL43712 — IC50 = 2900.0 nM 5.54
CHEMBL332137 — IC50 = 3160.0 nM 5.50
CHEMBL115515 — IC50 = 3500.0 nM 5.46
CHEMBL298199 — IC50 = 3600.0 nM 5.44
CHEMBL331185 — IC50 = 3600.0 nM 5.44